Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes. (4th November 2014)

• Record Type: Journal Article
• Authors: Krátký, Martin; Novotná, Eva; Saxena, Shalini; Yogeeswari, Perumal; Sriram, Dharmarajan; Švarcová, Markéta; Vinšová, Jarmila
• Other Names: Surguchov Andrei Academic Editor.
• Is Part Of: TheScientificWorldjournal. Volume 2014(2014)
• Publication Date: 2014-11-04
• Subjects: Science -- Periodicals; Technology -- Periodicals; Medicine -- Periodicals; 505
• DOI: 10.1155/2014/703053
• Languages: English
• ISSNs: 2356-6140

Abstract

Abstract : Antimycobacterially active salicylanilide diethyl phosphates were evaluated to identify their potential drug target(s) for the inhibition of several mycobacterial enzymes, including isocitrate lyase, L-alanine dehydrogenase ( Mt AlaDH), lysine ε -aminotransferase, chorismate mutase, and pantothenate synthetase. The enzymes are related to the nongrowing state of Mycobacterium tuberculosis . Salicylanilide diethyl phosphates represent new candidates with significant inhibitory activity especially against L-alanine dehydrogenase. The most active Mt AlaDH inhibitor, 5-chloro-2-[(3-chlorophenyl)carbamoyl]phenyl diethyl phosphate, has an IC50 of 4.96 µ M and the best docking results. Other mycobacterial enzymes were mostly inhibited by some derivatives but at higher concentrations; isocitrate lyase showed the highest resistance to salicylanilide diethyl phosphates.